Disease relevance of LOC404074

• Nordihydroguaiaretic acid (NDGA; a lipoxygenase inhibitor), LY-270766 (an inhibitor of 5-lipoxygenase), and the diacylglycerol lipase inhibitor RG 80267 completely eliminated potassium-evoked release of [3H]-noradrenaline ([3H]NA) from the human neuroblastoma clone SH-SY5Y with IC50 values of 10, 15, and 30 microM, respectively [1].
• The in vitro generation and release of 5-lipoxygenase metabolites of arachidonic acid by bovine peripheral blood neutrophils and alveolar neutrophils elicited with either a heat-killed bacterium, Haemophilus somnus, or platelet-activating factor, were compared [2].
• Influence of hypoxia on 5-lipoxygenase pathway in rat alveolar macrophages [3].
• Studies on lipoxygenase inhibitors. II. KF8940 (2-n-heptyl-4-hydroxyquinoline-N-oxide), a potent and selective inhibitor of 5-lipoxygenase, produced by Pseudomonas methanica [4].

High impact information on LOC404074

• A decade ago, we initiated studies to define relationship(s) between products of 5-lipoxygenase-mediated arachidonic acid metabolism and altered microvascular permeability [5].
• Incubation of circulating neutrophils with rbIL-1 beta and A23187 concurrently resulted in a significantly increased release of all 5-lipoxygenase metabolites of arachidonate [6].
• In vivo chemotaxis of bovine neutrophils induced by 5-lipoxygenase metabolites of arachidonic and eicosapentaenoic acid [7].
• The measurements of arterial plasma LTB indicate that indomethacin treatment alone, which inhibits cyclooxygenase activity, and FFD treatment each augment the metabolism of arachidonic acid by the 5-lipoxygenase pathway in animals pretreated with mepyramine.(ABSTRACT TRUNCATED AT 400 WORDS)[8]
• The 5-lipoxygenase inhibitor 5,6-dehydroarachidonic acid had no effect on vascular cell proliferation, but inhibition of 12-lipoxygenase with baicalein blocked both EC and SMC cell growth in a dose-dependent manner, in the presence and the absence of growth factors [9].

Chemical compound and disease context of LOC404074

• The synthesis of 5-HETE increased during hypoxia and the total production of LTB4, LTC4 and 5-HETE, the major metabolites of the 5-lipoxygenase pathway in rat alveolar macrophages, was equal during normoxia and hypoxia [3].
• In addition, the role of cyclooxygenase and 5-lipoxygenase metabolites of arachidonic acid in the potentiation evoked by AII, hypoxia or PDBu was studied, using indomethacin and nordihydroguaiaretic acid (NDGA) [10].

Biological context of LOC404074

• Structure-activity relationships have shown that the presence of free phenolic groups in the attached aromatic ring is beneficial but not required for 5-LO inhibitory potency [11].
• QSAR study of dual cyclooxygenase and 5-lipoxygenase inhibitors 2,6-di-tert-butylphenol derivatives [12].
• The iminoxy acetic acid derivative and the iminotetrazole selectively inhibit the 5-lipoxygenase, all the other compounds show medium or low affinity to the active sites of cyclooxygenase and 5-lipoxygenase [13].

Anatomical context of LOC404074

• These results show clearly that 5-lipoxygenase metabolites can initiate the extravascular accumulation of bovine neutrophils in vivo [7].
• A novel series of 2- and 3-substituted 1,8-dihydroxy-9(10H)-anthracenones were synthesized and tested for their inhibitory activity against 5-lipoxygenase (5-LO) in bovine polymorphonuclear leukocytes and the growth of human keratinocytes [14].
• Leukotriene A4, and not leukotriene B4, is the main 5-lipoxygenase metabolite released by bovine leukocytes [15].
• pH-dependent regulation of leukocyte 5-lipoxygenase activity in inflammatory exudates by albumin [16].
• AA861, a specific 5-lipoxygenase inhibitor, inhibited bovine lymphocyte response to phytohemagglutinin (PHA) [17].

Associations of LOC404074 with chemical compounds

• Circulating neutrophils, preincubated with rbIL-1 beta and stimulated with A23187, released significantly greater amounts of 5-hydroxyeicosatetraenoic acid and total 5-lipoxygenase metabolites when compared with control cells not incubated with rbIL-1 beta [6].
• Within a class of structural analogs the activity against 5-LO, which was markedly improved as compared to that of the antipsoriatic drug anthralin, correlated well with the overall lipophilicity [14].
• FPL 55712 and SKF 102922 and the 5-lipoxygenase inhibitor nordihydroguaiaretic acid (NDGA) had no effect on the response to antigen when used alone [18].
• However, several derivatives of this series maintained 5-LO inhibitory activity but did not generate hydroxyl radicals and were not reactive with DPPH [11].
• Treating silica with aluminum lactate or PVPNO significantly (P less than or equal to 0.05) reduced 5-lipoxygenase metabolite release and significantly (P less than or equal to 0.05) increased cyclooxygenase metabolite release [19].

Other interactions of LOC404074

• The antipsoriatic Mahonia aquifolium and its active constituents; I. Pro- and antioxidant properties and inhibition of 5-lipoxygenase [20].
• No significant increase in mRNA expression of platelet-activating factor acethylhydrolase, 5-lipoxygenase, and insulin-like growth factor 1 was found [21].
• The role of cyclooxygenase and 5-lipoxygenase metabolites in potentiated endothelin-1-evoked contractions in bovine bronchi [10].

Analytical, diagnostic and therapeutic context of LOC404074

• Finally, Northern blot analysis revealed mRNA for 5-lipoxygenase to be present in human and bovine PMNs, but not in BRPs [22].
• METHODS: Rat peritoneal leukocytes were isolated and the cellular 5-lipoxygenase activity was determined by HPLC after cell stimulation with calcium ionophore A23187 [16].

References